Synthesis and potential coanthracyclinic activity of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones

  title={Synthesis and potential coanthracyclinic activity of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones},
  author={Aldo Andreani and Alessandra Locatelli and Alberto Leoni and Mirella Rambaldi and Rita Morigi and Rosaria Bossa and Michele Chiericozzi and A Fraccari and Iraklis Galatulas},
  journal={European Journal of Medicinal Chemistry},

Imidazo[2,1 -b]thiazolylmethylene- and indolylmethylene-2-indolinones: a new class of cyclin-dependent kinase inhibitors. Design, synthesis, and CDK1/cyclin B inhibition.

(2-chloroindolyl)methylene-2-indolinone is identified as a new lead of a class of CDK1/cyclinB inhibitors, whose potency can be improved by the introduction of suitable variations on the basic molecular skeleton.

Substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones with antitumor activity. In depth study of the effect on growth of breast cancer cells.

The ability of these derivatives to inhibit cellular proliferation was accompanied by increased level of p53 and its transcriptional targets p21 and Bax, interference in the cell cycle progression with cell accumulation in the G2/M phase, and activation of apoptosis.

Synthesis and Biological Evaluation of Imidazo[2,1‐b][1,3,4]thiadiazole‐Linked Oxindoles as Potent Tubulin Polymerization Inhibitors

Treatment with these three compounds resulted in accumulation of cells in G2/M phase, inhibition of tubulin assembly, and increased cyclin‐B1 protein levels, as well as potent anti‐proliferative activity.

Studies With 2-Benzothiazolylacetonitrile: Synthesis of New 2-Thienylbenzothiazoles and N-Thienyl maleimide Derivatives

The synthesis of new 2-thienylbenzothiazoles and N-thienyl maleimide derivatives utilizing 2-benzothiazolyl acetonitrile 1 as starting component.

Bioactivity-guided mixed synthesis and evaluation of α-alkenyl-γ and δ-lactone derivatives as potential fungicidal agents

The present study provided a more detailed insight into the antifungal activity of the α-methylene-γ-butyrolactone substructure, which provided a potential expectation for the exploration of α-alkenyl- γ- butyrolACTone structures in agriculture.



Potential antitumor agents. 25 [1]. Synthesis and cytotoxic activity of 3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones.

The Knoevenagel reaction between 2-indolinones and 2-chloroindolaldehydes gave 3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones which were tested as potential antitumor agents on cultures of

Potential antitumor agents. 24. Synthesis and pharmacological behavior of imidazo[2,1-b]thiazole guanylhydrazones bearing at least one chlorine.

The synthesis of new derivatives which were tested for antitumor and positive inotropic activity were reported, and in most cases the cytotoxic data from the in vitro experiments (HeLa) were in agreement with the antitumors data in vivo (Ehrlich).

Cardiotonic Activity of 2,5‐Dimethoxyphenylimidazo[2,1‐b]‐thiazoles

Compound 10 shows a strong positive inotropic activity: it increases the myocardial contractility in normal and hypodynamic heart muscle.

Cinnamamide analogs as inhibitors of protein tyrosine kinases.

A novel series of non-peptide PTK inhibitors which have as characteristic active pharmacophore the cinnamamide moiety are described which offer an unique target for selective anticancer chemotherapy.

[Anti-tumor activity of indole derivatives (author's transl)].